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<p>Histone deacetylases (HDACs) are attractive therapeutic targets due to their established role in tumorigenesis. In this study, a series of naphthalene-based hydroxamate derivatives were designed and synthesized as novel HDAC inhibitors. Among them, compound <b>6e</b> showed excellent inhibitory activities against HDAC1 and 4T1 cancer cell line, and it also increased the levels of acetylated histones H3 and H4. Moreover, <b>6e</b> induced significant cell apoptosis and cycle arrest. Importantly, <b>6e</b> exhibited significant antitumor activity in the 4T1 orthotopic autograft mouse model. Collectively, these results identify the naphthalene-hydroxamate scaffold as a promising template for the development of novel HDAC-targeted anticancer agents.</p>

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Naphthalene-based hydroxamate HDAC inhibitors with anti-breast tumor activity

  • 期刊论文

  • 发表日期：

    2026年5月29日

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  • Hui Song,
  • Feng-Chao Wang,
  • Wan-Dong Liu,
  • Quan-Hao Wei,
  • Feifei Yang,
  • Peipei Shan,
  • Hua Zhang

摘要

Histone deacetylases (HDACs) are attractive therapeutic targets due to their established role in tumorigenesis. In this study, a series of naphthalene-based hydroxamate derivatives were designed and synthesized as novel HDAC inhibitors. Among them, compound 6e showed excellent inhibitory activities against HDAC1 and 4T1 cancer cell line, and it also increased the levels of acetylated histones H3 and H4. Moreover, 6e induced significant cell apoptosis and cycle arrest. Importantly, 6e exhibited significant antitumor activity in the 4T1 orthotopic autograft mouse model. Collectively, these results identify the naphthalene-hydroxamate scaffold as a promising template for the development of novel HDAC-targeted anticancer agents.